JP2005500319A5 - - Google Patents
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- JP2005500319A5 JP2005500319A5 JP2003508361A JP2003508361A JP2005500319A5 JP 2005500319 A5 JP2005500319 A5 JP 2005500319A5 JP 2003508361 A JP2003508361 A JP 2003508361A JP 2003508361 A JP2003508361 A JP 2003508361A JP 2005500319 A5 JP2005500319 A5 JP 2005500319A5
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- JP
- Japan
- Prior art keywords
- group
- substituted
- oxide
- unsubstituted
- alkoxy
- Prior art date
- Legal status (The legal status is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the status listed.)
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- -1 indazolylyl Thienyl Chemical group 0.000 claims 49
- 125000001424 substituent group Chemical group 0.000 claims 25
- 125000003545 alkoxy group Chemical group 0.000 claims 23
- 125000000217 alkyl group Chemical group 0.000 claims 22
- 150000001875 compounds Chemical class 0.000 claims 9
- 229910052717 sulfur Inorganic materials 0.000 claims 7
- 125000004435 hydrogen atoms Chemical group [H]* 0.000 claims 6
- 206010001897 Alzheimer's disease Diseases 0.000 claims 5
- 125000000882 C2-C6 alkenyl group Chemical group 0.000 claims 5
- 206010012289 Dementia Diseases 0.000 claims 5
- OKTJSMMVPCPJKN-UHFFFAOYSA-N carbon Chemical group [C] OKTJSMMVPCPJKN-UHFFFAOYSA-N 0.000 claims 5
- 229910052799 carbon Inorganic materials 0.000 claims 5
- 125000004429 atoms Chemical group 0.000 claims 4
- 125000000753 cycloalkyl group Chemical group 0.000 claims 4
- 229910052739 hydrogen Inorganic materials 0.000 claims 4
- 125000004857 imidazopyridinyl group Chemical group N1C(=NC2=C1C=CC=N2)* 0.000 claims 4
- IJGRMHOSHXDMSA-UHFFFAOYSA-N nitrogen Chemical compound N#N IJGRMHOSHXDMSA-UHFFFAOYSA-N 0.000 claims 4
- 125000004568 thiomorpholinyl group Chemical group 0.000 claims 4
- 125000001164 benzothiazolyl group Chemical group S1C(=NC2=C1C=CC=C2)* 0.000 claims 3
- 125000004600 benzothiopyranyl group Chemical group S1C(C=CC2=C1C=CC=C2)* 0.000 claims 3
- 150000002148 esters Chemical class 0.000 claims 3
- 125000003453 indazolyl group Chemical group N1N=C(C2=C1C=CC=C2)* 0.000 claims 3
- 125000002757 morpholinyl group Chemical group 0.000 claims 3
- 125000004193 piperazinyl group Chemical group 0.000 claims 3
- 125000003386 piperidinyl group Chemical group 0.000 claims 3
- 125000000719 pyrrolidinyl group Chemical group 0.000 claims 3
- 125000001422 pyrrolinyl group Chemical group 0.000 claims 3
- 125000002294 quinazolinyl group Chemical group N1=C(N=CC2=CC=CC=C12)* 0.000 claims 3
- 150000003839 salts Chemical class 0.000 claims 3
- 239000011780 sodium chloride Substances 0.000 claims 3
- 125000001637 1-naphthyl group Chemical group [H]C1=C([H])C([H])=C2C(*)=C([H])C([H])=C([H])C2=C1[H] 0.000 claims 2
- 125000001622 2-naphthyl group Chemical group [H]C1=C([H])C([H])=C2C([H])=C(*)C([H])=C([H])C2=C1[H] 0.000 claims 2
- 125000003785 benzimidazolyl group Chemical group N1=C(NC2=C1C=CC=C2)* 0.000 claims 2
- 125000002047 benzodioxolyl group Chemical group O1OC(C2=C1C=CC=C2)* 0.000 claims 2
- 125000004619 benzopyranyl group Chemical group O1C(C=CC2=C1C=CC=C2)* 0.000 claims 2
- 125000004196 benzothienyl group Chemical group S1C(=CC2=C1C=CC=C2)* 0.000 claims 2
- 125000004622 benzoxazinyl group Chemical group O1NC(=CC2=C1C=CC=C2)* 0.000 claims 2
- 125000004541 benzoxazolyl group Chemical group O1C(=NC2=C1C=CC=C2)* 0.000 claims 2
- 125000002837 carbocyclic group Chemical group 0.000 claims 2
- 125000004432 carbon atoms Chemical group C* 0.000 claims 2
- 125000003016 chromanyl group Chemical group O1C(CCC2=CC=CC=C12)* 0.000 claims 2
- 125000004617 chromonyl group Chemical group O1C(=CC(C2=CC=CC=C12)=O)* 0.000 claims 2
- 125000000332 coumarinyl group Chemical group O1C(=O)C(=CC2=CC=CC=C12)* 0.000 claims 2
- 230000003412 degenerative Effects 0.000 claims 2
- 125000005992 dihydrobenzisothiazinyl group Chemical group 0.000 claims 2
- 125000005993 dihydrobenzisoxazinyl group Chemical group 0.000 claims 2
- 125000005044 dihydroquinolinyl group Chemical group N1(CC=CC2=CC=CC=C12)* 0.000 claims 2
- 201000010099 disease Diseases 0.000 claims 2
- 239000003814 drug Substances 0.000 claims 2
- 125000001072 heteroaryl group Chemical group 0.000 claims 2
- 125000005842 heteroatoms Chemical group 0.000 claims 2
- 239000001257 hydrogen Substances 0.000 claims 2
- 125000002883 imidazolyl group Chemical group 0.000 claims 2
- 125000003392 indanyl group Chemical group C1(CCC2=CC=CC=C12)* 0.000 claims 2
- 125000003387 indolinyl group Chemical group N1(CCC2=CC=CC=C12)* 0.000 claims 2
- 125000001041 indolyl group Chemical group 0.000 claims 2
- 125000005994 isobenzotetrahydrofuranyl group Chemical group 0.000 claims 2
- 125000005990 isobenzothienyl group Chemical group 0.000 claims 2
- 125000003151 isocoumarinyl group Chemical group C1(=O)OC(=CC2=CC=CC=C12)* 0.000 claims 2
- 125000000904 isoindolyl group Chemical group C=1(NC=C2C=CC=CC12)* 0.000 claims 2
- 125000005956 isoquinolyl group Chemical group 0.000 claims 2
- 125000001786 isothiazolyl group Chemical group 0.000 claims 2
- 125000000842 isoxazolyl group Chemical group 0.000 claims 2
- 125000004593 naphthyridinyl group Chemical group N1=C(C=CC2=CC=CN=C12)* 0.000 claims 2
- 229910052757 nitrogen Inorganic materials 0.000 claims 2
- 125000001715 oxadiazolyl group Chemical group 0.000 claims 2
- 125000002971 oxazolyl group Chemical group 0.000 claims 2
- 239000008194 pharmaceutical composition Substances 0.000 claims 2
- 125000001484 phenothiazinyl group Chemical group C1(=CC=CC=2SC3=CC=CC=C3NC12)* 0.000 claims 2
- 125000001644 phenoxazinyl group Chemical group C1(=CC=CC=2OC3=CC=CC=C3NC12)* 0.000 claims 2
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 claims 2
- 125000004592 phthalazinyl group Chemical group C1(=NN=CC2=CC=CC=C12)* 0.000 claims 2
- 125000001042 pteridinyl group Chemical group N1=C(N=CC2=NC=CN=C12)* 0.000 claims 2
- 125000000561 purinyl group Chemical group N1=C(N=C2N=CNC2=C1)* 0.000 claims 2
- 125000003373 pyrazinyl group Chemical group 0.000 claims 2
- 125000003226 pyrazolyl group Chemical group 0.000 claims 2
- 125000002098 pyridazinyl group Chemical group 0.000 claims 2
- 125000004076 pyridyl group Chemical group 0.000 claims 2
- 125000000714 pyrimidinyl group Chemical group 0.000 claims 2
- 125000000168 pyrrolyl group Chemical group 0.000 claims 2
- 125000002943 quinolinyl group Chemical group N1=C(C=CC2=CC=CC=C12)* 0.000 claims 2
- 125000001567 quinoxalinyl group Chemical group N1=C(C=NC2=CC=CC=C12)* 0.000 claims 2
- 125000003039 tetrahydroisoquinolinyl group Chemical group C1(NCCC2=CC=CC=C12)* 0.000 claims 2
- 125000005958 tetrahydrothienyl group Chemical group 0.000 claims 2
- 125000005329 tetralinyl group Chemical group C1(CCCC2=CC=CC=C12)* 0.000 claims 2
- 125000003831 tetrazolyl group Chemical group 0.000 claims 2
- 125000001113 thiadiazolyl group Chemical group 0.000 claims 2
- 125000000335 thiazolyl group Chemical group 0.000 claims 2
- 125000004306 triazinyl group Chemical group 0.000 claims 2
- 125000001425 triazolyl group Chemical group 0.000 claims 2
- 125000004933 β-carbolinyl group Chemical group C1(=NC=CC=2C3=CC=CC=C3NC12)* 0.000 claims 2
- HPARLNRMYDSBNO-UHFFFAOYSA-N 1,4-Benzodioxine Chemical compound C1=CC=C2OC=COC2=C1 HPARLNRMYDSBNO-UHFFFAOYSA-N 0.000 claims 1
- GIIWGCBLYNDKBO-UHFFFAOYSA-N 1-oxidoquinolin-1-ium Chemical compound C1=CC=C2[N+]([O-])=CC=CC2=C1 GIIWGCBLYNDKBO-UHFFFAOYSA-N 0.000 claims 1
- 206010002022 Amyloidosis Diseases 0.000 claims 1
- 206010002023 Amyloidosis Diseases 0.000 claims 1
- 125000003601 C2-C6 alkynyl group Chemical group 0.000 claims 1
- 208000005145 Cerebral Amyloid Angiopathy Diseases 0.000 claims 1
- 206010008111 Cerebral haemorrhage Diseases 0.000 claims 1
- 206010057668 Cognitive disease Diseases 0.000 claims 1
- 201000010374 Down syndrome Diseases 0.000 claims 1
- 206010018987 Haemorrhage Diseases 0.000 claims 1
- GWVMLCQWXVFZCN-UHFFFAOYSA-N Isoindoline Chemical compound C1=CC=C2CNCC2=C1 GWVMLCQWXVFZCN-UHFFFAOYSA-N 0.000 claims 1
- 210000004558 Lewy Bodies Anatomy 0.000 claims 1
- 206010061536 Parkinson's disease Diseases 0.000 claims 1
- 206010048327 Supranuclear palsy Diseases 0.000 claims 1
- 206010044688 Trisomy 21 Diseases 0.000 claims 1
- 239000004480 active ingredient Substances 0.000 claims 1
- 150000001298 alcohols Chemical class 0.000 claims 1
- 125000003342 alkenyl group Chemical group 0.000 claims 1
- 125000003118 aryl group Chemical group 0.000 claims 1
- 125000000499 benzofuranyl group Chemical group O1C(=CC2=C1C=CC=C2)* 0.000 claims 1
- 230000000740 bleeding Effects 0.000 claims 1
- 231100000319 bleeding Toxicity 0.000 claims 1
- 125000000609 carbazolyl group Chemical group C1(=CC=CC=2C3=CC=CC=C3NC12)* 0.000 claims 1
- 230000001054 cortical Effects 0.000 claims 1
- 230000003111 delayed Effects 0.000 claims 1
- 125000004852 dihydrofuranyl group Chemical group O1C(CC=C1)* 0.000 claims 1
- 125000005045 dihydroisoquinolinyl group Chemical group C1(NC=CC2=CC=CC=C12)* 0.000 claims 1
- 125000005043 dihydropyranyl group Chemical group O1C(CCC=C1)* 0.000 claims 1
- 125000005051 dihydropyrazinyl group Chemical group N1(CC=NC=C1)* 0.000 claims 1
- 125000005052 dihydropyrazolyl group Chemical group N1(NCC=C1)* 0.000 claims 1
- 125000004655 dihydropyridinyl group Chemical group N1(CC=CC=C1)* 0.000 claims 1
- 125000005053 dihydropyrimidinyl group Chemical group N1(CN=CC=C1)* 0.000 claims 1
- 125000005054 dihydropyrrolyl group Chemical group [H]C1=C([H])C([H])([H])C([H])([H])N1* 0.000 claims 1
- 125000002541 furyl group Chemical group 0.000 claims 1
- 125000000623 heterocyclic group Chemical group 0.000 claims 1
- RCCPEORTSYDPMB-UHFFFAOYSA-N hydroxy benzenecarboximidothioate Chemical compound OSC(=N)C1=CC=CC=C1 RCCPEORTSYDPMB-UHFFFAOYSA-N 0.000 claims 1
- 125000003454 indenyl group Chemical group C1(C=CC2=CC=CC=C12)* 0.000 claims 1
- 125000003406 indolizinyl group Chemical group C=1(C=CN2C=CC=CC12)* 0.000 claims 1
- 125000005995 isobenzotetrahydrothienyl group Chemical group 0.000 claims 1
- 125000003384 isochromanyl group Chemical group C1(OCCC2=CC=CC=C12)* 0.000 claims 1
- 125000004594 isoindolinyl group Chemical group C1(NCC2=CC=CC=C12)* 0.000 claims 1
- 229910052760 oxygen Inorganic materials 0.000 claims 1
- 230000000306 recurrent Effects 0.000 claims 1
- 125000003718 tetrahydrofuranyl group Chemical group 0.000 claims 1
- 125000001412 tetrahydropyranyl group Chemical group 0.000 claims 1
- 125000000147 tetrahydroquinolinyl group Chemical group N1(CCCC2=CC=CC=C12)* 0.000 claims 1
- 125000001544 thienyl group Chemical group 0.000 claims 1
- 230000002792 vascular Effects 0.000 claims 1
Applications Claiming Priority (4)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US30121001P | 2001-06-27 | 2001-06-27 | |
| US32339601P | 2001-09-18 | 2001-09-18 | |
| US33273601P | 2001-11-19 | 2001-11-19 | |
| PCT/US2002/020754 WO2003002122A1 (en) | 2001-06-27 | 2002-06-27 | Beta-hydroxyamine derivatives useful in treatment of alzheimer's disease |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| JP2005500319A JP2005500319A (ja) | 2005-01-06 |
| JP2005500319A5 true JP2005500319A5 (es) | 2006-01-05 |
Family
ID=27404798
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2003508361A Pending JP2005500319A (ja) | 2001-06-27 | 2002-06-27 | アルツハイマー病の治療に有用なβ−ヒドロキシアミン誘導体 |
Country Status (7)
| Country | Link |
|---|---|
| US (2) | US6982264B2 (es) |
| EP (1) | EP1401452A1 (es) |
| JP (1) | JP2005500319A (es) |
| BR (1) | BR0210721A (es) |
| CA (1) | CA2452039A1 (es) |
| MX (1) | MXPA04000140A (es) |
| WO (1) | WO2003002122A1 (es) |
Families Citing this family (33)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US7521481B2 (en) | 2003-02-27 | 2009-04-21 | Mclaurin Joanne | Methods of preventing, treating and diagnosing disorders of protein aggregation |
| US20050239836A1 (en) | 2004-03-09 | 2005-10-27 | Varghese John | Substituted hydroxyethylamine aspartyl protease inhibitors |
| WO2007047305A1 (en) | 2005-10-12 | 2007-04-26 | Elan Pharmaceuticals, Inc. | Methods of treating amyloidosis using cyclopropyl derivative aspartyl protease inhibitors |
| US7872009B2 (en) | 2005-11-21 | 2011-01-18 | Amgen Inc. | Beta-Secretase modulators and methods of use |
| JP5274258B2 (ja) | 2005-11-21 | 2013-08-28 | アムジエン・インコーポレーテツド | β−セクレターゼ調節物質及び使用方法 |
| US7745484B2 (en) * | 2005-11-21 | 2010-06-29 | Amgen Inc. | Beta-secretase modulators and methods of use |
| US7838676B2 (en) * | 2005-11-21 | 2010-11-23 | Amgen Inc. | Beta-secretase modulators and methods of use |
| WO2008055945A1 (en) | 2006-11-09 | 2008-05-15 | Probiodrug Ag | 3-hydr0xy-1,5-dihydr0-pyrr0l-2-one derivatives as inhibitors of glutaminyl cyclase for the treatment of ulcer, cancer and other diseases |
| WO2008065141A1 (en) | 2006-11-30 | 2008-06-05 | Probiodrug Ag | Novel inhibitors of glutaminyl cyclase |
| ZA200905537B (en) | 2007-03-01 | 2010-10-27 | Probiodrug Ag | New use of glutaminyl cyclase inhibitors |
| JP5667440B2 (ja) | 2007-04-18 | 2015-02-12 | プロビオドルグ エージー | グルタミニルシクラーゼ阻害剤としてのチオ尿素誘導体 |
| WO2008137168A2 (en) * | 2007-05-07 | 2008-11-13 | True Charles W | Collapsible, stackable, semi-rigid universal tank for hazardous and non-hazardous goods |
| US8173810B2 (en) * | 2007-05-25 | 2012-05-08 | Amgen Inc. | Substituted hydroxyethyl amine compounds as beta-secretase modulators and methods of use |
| US8163909B2 (en) | 2007-05-25 | 2012-04-24 | Amgen Inc. | Substituted hydroxyethyl amine compounds as beta-secretase modulators and methods of use |
| US7803809B2 (en) | 2008-11-12 | 2010-09-28 | Amgen Inc. | Substituted pyrano [2,3-b] pyridinamine compounds as beta-secretase modulators and methods of use |
| WO2009076352A1 (en) * | 2007-12-11 | 2009-06-18 | Schering Corporation | Gamma secretase modulators |
| EP3403650A3 (en) | 2008-07-28 | 2019-02-13 | Blanchette Rockefeller Neurosciences, Institute | Pkc-activating compounds for the treatment of neurodegenerative diseases |
| CA2736130C (en) * | 2008-09-11 | 2014-01-14 | Amgen Inc. | Spiro-tetracyclic ring compounds as beta-secretase modulators and methods of use |
| MX2012002993A (es) | 2009-09-11 | 2012-04-19 | Probiodrug Ag | Derivados heterociclicos como inhibidores de ciclasa glutaminilo. |
| WO2011063233A1 (en) | 2009-11-23 | 2011-05-26 | Amgen Inc. | Amino heteroaryl compounds as beta-secretase modulators and methods of use |
| WO2011063272A1 (en) | 2009-11-23 | 2011-05-26 | Amgen Inc. | Amino heteroaryl compounds as beta-secretase modulators and methods of use |
| EP2526092B1 (en) | 2010-01-19 | 2014-08-06 | Amgen Inc. | Amino heteroaryl compounds as beta-secretase modulators and methods of use |
| JP6026284B2 (ja) | 2010-03-03 | 2016-11-16 | プロビオドルグ エージー | グルタミニルシクラーゼの阻害剤 |
| MX2012010470A (es) | 2010-03-10 | 2012-10-09 | Probiodrug Ag | Inhibidores heterociclicos d ciclasa de glutaminilo (qc, ec .3 2. 5). |
| US8497264B2 (en) | 2010-03-15 | 2013-07-30 | Amgen Inc. | Amino-oxazines and amino-dihydrothiazine compounds as beta-secretase modulators and methods of use |
| US8883782B2 (en) | 2010-03-15 | 2014-11-11 | Amgen Inc. | Spiro-tetracyclic ring compounds as beta-secretase modulators and methods of use |
| US8541596B2 (en) | 2010-04-21 | 2013-09-24 | Probiodrug Ag | Inhibitors |
| US9346827B2 (en) | 2011-02-07 | 2016-05-24 | Amgen Inc. | 5-amino-oxazepine and 5-amino-thiazepane compounds as beta secretase antagonists and methods of use |
| WO2012123563A1 (en) | 2011-03-16 | 2012-09-20 | Probiodrug Ag | Benz imidazole derivatives as inhibitors of glutaminyl cyclase |
| WO2013044092A1 (en) | 2011-09-21 | 2013-03-28 | Amgen Inc. | Amino-oxazines and amino-dihydrothiazine compounds as beta-secretase modulators and methods of use |
| US9725469B2 (en) | 2012-11-15 | 2017-08-08 | Amgen, Inc. | Amino-oxazine and amino-dihydrothiazine compounds as beta-secretase modulators and methods of use |
| US20140249377A1 (en) * | 2013-03-01 | 2014-09-04 | Eugen Tarnow | Well defined system and method for monitoring neurological disease onset and progress and onset of the effects of neuropharmacological drugs using the recency-primacy shift and overall free recall differences |
| EP3461819B1 (en) | 2017-09-29 | 2020-05-27 | Probiodrug AG | Inhibitors of glutaminyl cyclase |
Family Cites Families (109)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US3547119A (en) | 1967-12-08 | 1970-12-15 | Baxter Laboratories Inc | Catheter assembly |
| US3739778A (en) * | 1971-08-12 | 1973-06-19 | Bard Inc C R | Catheter introduction system |
| US3996923A (en) | 1973-03-23 | 1976-12-14 | Guerra Luis A | Blood taking device |
| US4106491A (en) * | 1975-07-24 | 1978-08-15 | Guerra Luis A | Device for prolonged intravascular infusion |
| JPS5753564Y2 (es) | 1977-06-01 | 1982-11-19 | ||
| US4126133A (en) | 1977-07-13 | 1978-11-21 | Boris Schwartz | Intracorporeal catheter improvement |
| CH624011A5 (es) * | 1977-08-05 | 1981-07-15 | Battelle Memorial Institute | |
| FR2416008A1 (fr) * | 1978-02-02 | 1979-08-31 | Oreal | Lyophilisats de liposomes |
| US4235871A (en) | 1978-02-24 | 1980-11-25 | Papahadjopoulos Demetrios P | Method of encapsulating biologically active materials in lipid vesicles |
| US4394448A (en) * | 1978-02-24 | 1983-07-19 | Szoka Jr Francis C | Method of inserting DNA into living cells |
| DE2845643C2 (de) * | 1978-10-20 | 1982-04-08 | Max Dr. 8520 Erlangen Hubmann | Katheteranschlußkopf mit mindestens einem Kanal in einem Grundkörper |
| US4258940A (en) * | 1979-03-01 | 1981-03-31 | Bio-Dynamics, Inc. | Sealing connector for liquid and gas systems |
| US4399216A (en) * | 1980-02-25 | 1983-08-16 | The Trustees Of Columbia University | Processes for inserting DNA into eucaryotic cells and for producing proteinaceous materials |
| US4311137A (en) * | 1980-04-30 | 1982-01-19 | Sherwood Medical Industries Inc. | Infusion device |
| US5142056A (en) * | 1989-05-23 | 1992-08-25 | Abbott Laboratories | Retroviral protease inhibiting compounds |
| US4430081A (en) * | 1981-01-06 | 1984-02-07 | Cook, Inc. | Hemostasis sheath |
| US4418944A (en) | 1981-02-11 | 1983-12-06 | Haines Stephen W | Fluid coupling |
| US4522811A (en) * | 1982-07-08 | 1985-06-11 | Syntex (U.S.A.) Inc. | Serial injection of muramyldipeptides and liposomes enhances the anti-infective activity of muramyldipeptides |
| US4870009A (en) * | 1982-11-22 | 1989-09-26 | The Salk Institute For Biological Studies | Method of obtaining gene product through the generation of transgenic animals |
| US4668770A (en) * | 1982-12-27 | 1987-05-26 | Merck & Co., Inc. | Renin inhibitory tripeptides |
| US5281206A (en) * | 1983-01-24 | 1994-01-25 | Icu Medical, Inc. | Needle connector with rotatable collar |
| US4531937A (en) * | 1983-01-24 | 1985-07-30 | Pacesetter Systems, Inc. | Introducer catheter apparatus and method of use |
| US5330450A (en) * | 1983-01-24 | 1994-07-19 | Icu Medical, Inc. | Medical connector |
| US4816567A (en) | 1983-04-08 | 1989-03-28 | Genentech, Inc. | Recombinant immunoglobin preparations |
| US4636491A (en) * | 1984-03-27 | 1987-01-13 | Merck & Co., Inc. | Renin inhibitory peptides having improved solubility |
| US4736866A (en) * | 1984-06-22 | 1988-04-12 | President And Fellows Of Harvard College | Transgenic non-human mammals |
| US4880781A (en) | 1984-08-06 | 1989-11-14 | The Upjohn Company | Renin inhibitory peptides containing an N-alkyl-histidine moiety |
| JPS6150912A (ja) * | 1984-08-16 | 1986-03-13 | Shionogi & Co Ltd | リポソ−ム製剤の製造法 |
| US4814270A (en) * | 1984-09-13 | 1989-03-21 | Becton Dickinson And Company | Production of loaded vesicles |
| US4749792A (en) * | 1984-09-26 | 1988-06-07 | E. R. Squibb & Sons, Inc. | Diamino ketones and alcohols as analgesic agents |
| US4616088A (en) | 1984-10-29 | 1986-10-07 | E. R. Squibb & Sons, Inc. | Amino acid ester and amide renin inhibitor |
| US4665193A (en) * | 1984-12-14 | 1987-05-12 | E. R. Squibb & Sons, Inc. | Amino acid ester renin inhibitors |
| US4897355A (en) * | 1985-01-07 | 1990-01-30 | Syntex (U.S.A.) Inc. | N[ω,(ω-1)-dialkyloxy]- and N-[ω,(ω-1)-dialkenyloxy]-alk-1-yl-N,N,N-tetrasubstituted ammonium lipids and uses therefor |
| US4753788A (en) * | 1985-01-31 | 1988-06-28 | Vestar Research Inc. | Method for preparing small vesicles using microemulsification |
| US4645495A (en) * | 1985-06-26 | 1987-02-24 | Vaillancourt Vincent L | Vascular access implant needle patch |
| US5175281A (en) | 1985-09-12 | 1992-12-29 | The Upjohn Company | Pharmaceutically active pyrimidinylpiperazinylsterioids |
| US4676980A (en) * | 1985-09-23 | 1987-06-30 | The United States Of America As Represented By The Secretary Of The Department Of Health And Human Services | Target specific cross-linked heteroantibodies |
| US4755173A (en) * | 1986-02-25 | 1988-07-05 | Pacesetter Infusion, Ltd. | Soft cannula subcutaneous injection set |
| US5250565A (en) | 1987-02-10 | 1993-10-05 | Abbott Laboratories | Indole-,benzofuran-,and benzothiophene-containing lipoxygenase-inhibiting compounds |
| US5010182A (en) * | 1987-07-28 | 1991-04-23 | Chiron Corporation | DNA constructs containing a Kluyveromyces alpha factor leader sequence for directing secretion of heterologous polypeptides |
| US5019054A (en) * | 1989-11-06 | 1991-05-28 | Mectra Labs, Inc. | Medical device valving mechanism |
| DE3941235A1 (de) | 1989-12-14 | 1991-06-20 | Bayer Ag | Neue peptide, ihre herstellung und ihre verwendung in arzneimitteln |
| GB9004483D0 (en) | 1990-02-28 | 1990-04-25 | Erba Carlo Spa | New aryl-and heteroarylethenylene derivatives and process for their preparation |
| US5098394A (en) * | 1990-05-31 | 1992-03-24 | Luther Ronald B | Biased shut off valve assembly for needle and catheter |
| US5912410A (en) * | 1990-06-15 | 1999-06-15 | Scios Inc. | Transgenic non-human mice displaying the amyloid-forming pathology of alzheimer's disease |
| EP0647268B1 (en) * | 1990-06-15 | 2004-03-03 | Scios Inc. | Transgenic non-human mammal displaying the amyloid-forming pathology of alzheimer's disease |
| US5176662A (en) * | 1990-08-23 | 1993-01-05 | Minimed Technologies, Ltd. | Subcutaneous injection set with improved cannula mounting arrangement |
| US5482947A (en) * | 1990-11-19 | 1996-01-09 | Talley; John J. | Retroviral protease inhibitors |
| US5648511A (en) * | 1990-11-19 | 1997-07-15 | G.D. Searle & Co. | Method for making intermediates useful in the synthesis of retroviral protease inhibitors |
| US5510487A (en) * | 1990-11-19 | 1996-04-23 | G.D. Searle & Co. | Retroviral protease inhibitors |
| DE69233774D1 (de) * | 1991-01-21 | 2009-12-10 | Elan Pharm Inc | Prüfung und Modell für Alzheimers-Krankheit |
| US5145684A (en) * | 1991-01-25 | 1992-09-08 | Sterling Drug Inc. | Surface modified drug nanoparticles |
| US5206161A (en) | 1991-02-01 | 1993-04-27 | Genentech, Inc. | Human plasma carboxypeptidase B |
| US5753652A (en) * | 1991-07-03 | 1998-05-19 | Novartis Corporation | Antiretroviral hydrazine derivatives |
| US5516784A (en) * | 1991-08-13 | 1996-05-14 | Schering Corporation | Anti-HIV (AIDS) agents |
| WO1993014200A1 (en) * | 1992-01-07 | 1993-07-22 | Tsi Corporation | Transgenic animal models for alzheimer's disease |
| DE69300043T2 (de) * | 1992-03-13 | 1995-05-24 | Bio Mega Boehringer Ingelheim | Substituierte Pipecoline-Säurederivate als HIV-Protease-Hemmer. |
| US5502187A (en) * | 1992-04-03 | 1996-03-26 | The Upjohn Company | Pharmaceutically active bicyclic-heterocyclic amines |
| US5441870A (en) * | 1992-04-15 | 1995-08-15 | Athena Neurosciences, Inc. | Methods for monitoring cellular processing of β-amyloid precursor protein |
| US5604102A (en) * | 1992-04-15 | 1997-02-18 | Athena Neurosciences, Inc. | Methods of screening for β-amyloid peptide production inhibitors |
| US5376542A (en) | 1992-04-27 | 1994-12-27 | Georgetown University | Method for producing immortalized cell lines using human papilluma virus genes |
| US5766846A (en) * | 1992-07-10 | 1998-06-16 | Athena Neurosciences | Methods of screening for compounds which inhibit soluble β-amyloid peptide production |
| US5843946A (en) * | 1992-08-25 | 1998-12-01 | G.D. Searle & Co. | α-and β-amino acid hydroxyethylamino sulfonamides useful as retroviral protease inhibitors |
| US5760076A (en) * | 1992-08-25 | 1998-06-02 | G.D Searle & Co. | Succinoylamino hydroxyethylamino sulfonamides useful as retroviral protease inhibitors |
| JP4091654B2 (ja) * | 1992-08-25 | 2008-05-28 | ジー．ディー．サール、リミテッド、ライアビリティ、カンパニー | レトロウイルスプロテアーゼ阻害剤として有用なスルホニルアルカノイルアミノヒドロキシエチルアミノスルホンアミド |
| US5830897A (en) | 1992-08-27 | 1998-11-03 | G. D. Searle & Co. | α- and β-amino acid hydroxyethylamino sulfonamides useful as retroviral protease inhibitors |
| US5578606A (en) * | 1992-10-30 | 1996-11-26 | G. D. Searle & Co. | α- and β-amino acid hydroxyethylamino sulfonyl urea derivatives useful as retroviral protease inhibitors |
| EP0604182B1 (en) * | 1992-12-22 | 2000-10-11 | Eli Lilly And Company | Inhibitors of HIV protease useful for the treatment of Aids |
| US5484926A (en) | 1993-10-07 | 1996-01-16 | Agouron Pharmaceuticals, Inc. | HIV protease inhibitors |
| US5545143A (en) * | 1993-01-21 | 1996-08-13 | T. S. I. Medical | Device for subcutaneous medication delivery |
| US5461067A (en) | 1993-02-25 | 1995-10-24 | Abbott Laboratories | Retroviral protease inhibiting compounds |
| US5257980A (en) | 1993-04-05 | 1993-11-02 | Minimed Technologies, Ltd. | Subcutaneous injection set with crimp-free soft cannula |
| US5300045A (en) * | 1993-04-14 | 1994-04-05 | Plassche Jr Walter M | Interventional needle having an automatically capping stylet |
| US5427145A (en) * | 1993-10-07 | 1995-06-27 | Abbott Laboratories | Connector with integral valve |
| CA2132277C (en) | 1993-10-22 | 2005-05-10 | Giorgio Cirelli | Injection device |
| ATE198622T1 (de) | 1993-10-27 | 2001-01-15 | Elan Pharm Inc | Transgene tiere, die app allele mit der schwedischen mutation beherbergen |
| US5733882A (en) * | 1994-01-17 | 1998-03-31 | Smithkline Beecham Corporation | Retroviral protease inhibitors |
| US5877399A (en) * | 1994-01-27 | 1999-03-02 | Johns Hopkins University | Transgenic mice expressing APP-Swedish mutation develop progressive neurologic disease |
| US5625031A (en) * | 1994-02-08 | 1997-04-29 | Bristol-Myers Squibb Company | Peptide inhibitors of the p33cdk2 and p34cdc2 cell cycle regulatory kinases and human papillomavirus E7 oncoprotein |
| US5475138A (en) * | 1994-07-07 | 1995-12-12 | Pharm-Eco Laboratories Incorporated | Method preparing amino acid-derived diaminopropanols |
| ATE220661T1 (de) * | 1994-10-19 | 2002-08-15 | Novartis Erfind Verwalt Gmbh | Antivirale ether von aspartat-protease-substrat- isosteren |
| DE4442352C1 (de) * | 1994-11-29 | 1995-12-21 | Braun Melsungen Ag | Ventilvorrichtung |
| US5481011A (en) * | 1994-12-13 | 1996-01-02 | Bristol-Myers Squibb Company | Process for preparing N-protected amino acid α-halomethyl ketones and alcohols from N-protected amino acid esters |
| US5804560A (en) * | 1995-01-06 | 1998-09-08 | Sibia Neurosciences, Inc. | Peptide and peptide analog protease inhibitors |
| US6017887A (en) * | 1995-01-06 | 2000-01-25 | Sibia Neurosciences, Inc. | Peptide, peptide analog and amino acid analog protease inhibitors |
| US5831117A (en) | 1995-01-20 | 1998-11-03 | G. D. Searle & Co. | Method of preparing retroviral protease inhibitor intermediates |
| ATE272069T1 (de) * | 1995-01-27 | 2004-08-15 | Novo Nordisk As | Verbindungen mit wachstumshormon-freisetzenden eigenschaften |
| US5545640A (en) * | 1995-04-04 | 1996-08-13 | Bio-Mega/Boehringer Ingeleheim Research Inc. | Protease inhibiting succinic acid derivatives |
| US5565483A (en) * | 1995-06-07 | 1996-10-15 | Bristol-Myers Squibb Company | 3-substituted oxindole derivatives as potassium channel modulators |
| US5942400A (en) * | 1995-06-07 | 1999-08-24 | Elan Pharmaceuticals, Inc. | Assays for detecting β-secretase |
| US5744346A (en) * | 1995-06-07 | 1998-04-28 | Athena Neurosciences, Inc. | β-secretase |
| IE77523B1 (en) * | 1995-09-11 | 1997-12-17 | Elan Med Tech | Medicament delivery device |
| US5858001A (en) * | 1995-12-11 | 1999-01-12 | Elan Medical Technologies Limited | Cartridge-based drug delivery device |
| US5849911A (en) | 1996-04-22 | 1998-12-15 | Novartis Finance Corporation | Antivirally active heterocyclic azahexane derivatives |
| JP2000509717A (ja) | 1996-05-07 | 2000-08-02 | ベーリンガー インゲルハイム ファーマシューティカルズ インコーポレイテッド | オキシランメタンアミン誘導体の調製方法 |
| DE69734215T2 (de) * | 1996-07-22 | 2006-06-29 | Novo Nordisk A/S | Verbindungen mit Wachstumshormon-freisetzenden Eigenschaften |
| US5703129A (en) * | 1996-09-30 | 1997-12-30 | Bristol-Myers Squibb Company | 5-amino-6-cyclohexyl-4-hydroxy-hexanamide derivatives as inhibitors of β-amyloid protein production |
| US6191166B1 (en) * | 1997-11-21 | 2001-02-20 | Elan Pharmaceuticals, Inc. | Methods and compounds for inhibiting β-amyloid peptide release and/or its synthesis |
| US6093172A (en) * | 1997-02-05 | 2000-07-25 | Minimed Inc. | Injector for a subcutaneous insertion set |
| US6045829A (en) * | 1997-02-13 | 2000-04-04 | Elan Pharma International Limited | Nanocrystalline formulations of human immunodeficiency virus (HIV) protease inhibitors using cellulosic surface stabilizers |
| TR199902056T2 (xx) * | 1997-02-26 | 2000-01-21 | Pfizer Inc. | Heteroaril-Heksanoik asit amid t�revleri. |
| US6221670B1 (en) * | 1997-03-21 | 2001-04-24 | Scios Inc. | Methods to identify β-amyloid reducing agents |
| US6186982B1 (en) * | 1998-05-05 | 2001-02-13 | Elan Corporation, Plc | Subcutaneous drug delivery device with improved filling system |
| US6213973B1 (en) * | 1998-01-12 | 2001-04-10 | C. R. Bard, Inc. | Vascular access port with elongated septum |
| US6095997A (en) * | 1998-03-04 | 2000-08-01 | Corvascular, Inc. | Intraluminal shunt and methods of use |
| US6056718A (en) * | 1998-03-04 | 2000-05-02 | Minimed Inc. | Medication infusion set |
| US6355021B1 (en) * | 1998-07-14 | 2002-03-12 | Maersk Medical A/S | Medical puncturing device |
| US6419699B1 (en) * | 1999-04-14 | 2002-07-16 | Mcghan Medical Corporation | Universal implant fill connector |
| CA2401749A1 (en) * | 2000-03-23 | 2001-09-27 | Elan Pharmaceuticals, Inc. | Compounds and methods to treat alzheimer's disease |
-
2002
- 2002-06-27 WO PCT/US2002/020754 patent/WO2003002122A1/en active Application Filing
- 2002-06-27 CA CA002452039A patent/CA2452039A1/en not_active Abandoned
- 2002-06-27 JP JP2003508361A patent/JP2005500319A/ja active Pending
- 2002-06-27 US US10/183,126 patent/US6982264B2/en not_active Expired - Fee Related
- 2002-06-27 MX MXPA04000140A patent/MXPA04000140A/es not_active Application Discontinuation
- 2002-06-27 EP EP02744767A patent/EP1401452A1/en not_active Withdrawn
- 2002-06-27 BR BR0210721-0A patent/BR0210721A/pt not_active IP Right Cessation
-
2006
- 2006-01-03 US US11/324,678 patent/US20060178345A1/en not_active Abandoned
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